Process for the preparation of a solid dosage form, in particular a tablet, for pharmaceutical use and process for the preparation of a precursor for a solid dosage form, in particular a tablet

a technology of solid dosage form and process, which is applied in the field of solid dosage form preparation process, can solve the problems of not being able to melt the entire formulation in order to achieve homogenous mixing, and achieve the effect of reducing the number of tablets

Active Publication Date: 2011-04-07
GRUNENTHAL GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For some solid formulations it might even be desirable to homogenously incorporate therein less than 1%, even less than 0.5 wt-% o

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Spray Congealed Powder Having the Following Composition

[0120]

DL-alpha-tocopherol (Vitamin E) 4.00 wt-%Polyethylene Glycol 6000 (PEG 6000)96.00 wt-%

Melt Preparation Process:

[0121]The required amounts of Vitamin E and PEG 6000 were weighed out. An appropriately sized stainless steel feed tank with mixer fitted with a Chromalox Micro Therm temperature control system was purged with nitrogen. PEG 6000 was slowly added into the feed tank. Once partially melted, it was agitated with a mixer to promote melting. Once PEG 6000 was completely added and melted, a melt temperature of 80° C. was maintained. The tank was continuously purged with nitrogen. Vitamin E was added into the molten PEG 6000. It was continued to mix for at least 10 minutes before spray congealing started. Agitation was kept throughout the spray congealing process.

Spray Congealing Process:

[0122]The thermal controllers for the feed lines were set at 90° C. and pre-heated for at least 30 minutes.

[0123]The spra...

example 2

Comparative Examples

Preparation of Powder Containing Vitamin E

[0125]The aim was to divide a small amount of vitamin E into a powder blend. The powder blend consisted of Tapentadol HCl, Polyethylene Oxide 7M, Hydroxypropyl methylcellulose and Polyethylene glycol 6000.

a)) Absorbing Vitamin E on a Solid Carrier

[0126]One way of incorporating a small amount of a liquid such as Vitamin E into a powder is first absorbing the liquid to a solid carrier, then blending with the remaining of the solid excipients. If the dilution is important, it can be performed geometrically, e.g. the Vitamin E containing carrier is mixed with one or more solid powder(s) (to obtain a certain dilution) and the blend obtained is diluted again with the same or other solid powder(s).

[0127]First it was tried to absorb the vitamin E on one of the excipients, namely polyethylene oxide PEO) 7 M which is a major component of the powder blend. It was tried to coat 1 part of Vitamin E on 9 parts of PEO. Distribution of t...

example 3

Spray Congealing Vitamin E and PEG 6000

[0143]PEG 6000 was weighed and molten on an off-line heating plate. Only slightly before the experiments took place an appropriate amount of Vitamin E was added and mechanically mixed with the PEG 6000. The mixture was heated to about 75 to 80° C. and transferred to the spraying nozzle of a Mobile Minor spray dryer by heated feed lines.

[0144]The mixture was sprayed through a two-fluid nozzle with N2 pre-heated at 100° C. The cooling gas was also N2 which had an in-let temperature of 11 to 13° C. and out-let temperature in the range of 20-26° C. After spraying the particles were collected in the cyclone of the spray-dryer.

[0145]Experiments were conducted with different concentrations of Vitamin E (1%, 2% or 4% (w / w) of actual Vitamin E content. Spray congealing of the Vitamin E with PEG 6000 was successful. The spray congealed product was obtained in a finely powdered state without being sticky or having much agglomeration. Loss of product in th...

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Abstract

Process for preparing a powder comprising the steps of providing at least one first component in liquid form at ambient temperature, providing at least one second component having a melting point or melting range in the range from above ambient temperature to below the degradation temperature of said first component, forming a homogenous liquid mixture comprising the at least one first component and the at least one second component by stirring and heating the mixture to or keeping the mixture at a temperature in the range from above the melting point or melting range of the second component and below the degradation temperature of the first component, transferring the liquid mixture to at least one spray congealing unit, spray congealing the mixture, and isolating the powder obtained upon spray congealing.

Description

[0001]The present invention pertains to a process of homogenously distributing a liquid, in particular a relatively small amount of a liquid, more in particular a relatively small amount of an oily substance, within a solid material so that a powder product is obtained which is suited to be used in the manufacture of a pharmaceutical composition, in particular a solid dosage form, such as for example a tablet, comprising at least one pharmaceutically active ingredient. The invention further pertains to a process for preparing a solid dosage form, such as a tablet, for pharmaceutical use.BACKGROUND OF THE INVENTION[0002]Usually, with solid oral dosage forms all excipients have to be homogenously distributed therein. Whereas typically solid excipients, irrespective of their relative amounts, can be homogenously mixed without facing any significant problems, it is rather critical to homogenously distribute liquids, more in particular relatively small amounts of an oil, in a solid mixtu...

Claims

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Application Information

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IPC IPC(8): A61K31/137A61K47/22A61P29/00B29B9/00B29B9/08
CPCA61K9/145A61K9/146A61K9/1617A61K9/2095A61K9/1694A61K9/2013A61K9/2031A61K9/1641A61P29/00
Inventor FAURE, ANNEVOORSPOELS, JODY FIRIM MARCELINEMERTENS, ROEL JOS M.KIEKENS, FILIP RENE IRENA
Owner GRUNENTHAL GMBH
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